Laropiprant


CAS No. : 571170-77-9

(Synonyms: MK-0524)

571170-77-9
Price and Availability of CAS No. : 571170-77-9
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5mg $120 In-stock
10mg $190 In-stock
25mg $310 In-stock
50mg $450 In-stock
100mg $680 In-stock
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Cat. No. : HY-50175
M.Wt: 435.90
Formula: C21H19ClFNO4S
Purity: >98 %
Solubility: DMSO : ≥ 100 mg/mL
Introduction of 571170-77-9 :

Laropiprant is a potent and selective DP receptor antagonist with Ki values of 0.57 nM and 2.95 nM for DP receptor and TP Receptor, respectively[1][2][3]. IC50 & Target:Ki: 0.57 nM (DP receptor)[1] In Vitro:Laropiprant (0.01-1000 μM; 10 mins; HEK293 cells) is an inverse agonist of DP1 cAMP signaling and reduces DP1 cAMP signaling below basal levels[1].
Laropiprant (1 μM; 0-24 h; HEK293 cells) is a pharmacochaperone in promoting DP1 cell surface expression[1]. In Vivo:Laropiprant (0-100 mg/kg; p.o. and i.v.; male Sprague-Dawley rats) exhibits good pharmacokinetic profiles[3].

Pharmacokinetic Analysis in Male Sprague-Dawley rats[3]
Route Dose (mg/kg) AUC0-∞ (μM·hr) Clp (mL/min/kg) Vdss (L/kg) T1/2 (hr)
PO 1 22.7 1.9 0.7 7.4
PO 5 96.0 2.1 0.9 7.6
Route Dose (mg/kg) AUC0-∞ (μM·hr) Cmax (μM) Tmax (hr) F(%)
IV 5 52.6 15.6 1.2 /

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